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Four new eudesmanolides and two new guaianolides were isolated from the aerial parts of Anthemis carpatica Willd. and their structures elucidated by spectral methods. In addition, seven known sesquiterpene lactones were identified.
Two Brazilian species of Dimerostemma (Asteraceae) were chemically investigated. Two known sesquiterpene lactones (STLs), a germacrolide and an eudesmanolide, were isolated from D. episcopale while D. brasilianum afforded the new germacranolide 1beta,5beta/10alpha-trihy-droxy-8alpha-angeloyloxy-germacra-3,11(13)-dien-6alpha,12-olide in addition to a known one. Structure identification based on NMR and MS analyses. 1beta,10alpha,4alpha,5beta-Diepoxy-8alpha-angeloyloxy-costunolide isolated from D. brasilianum was studied for its anti-inflammatory activity. This STL completely inhibited DNA binding of the transcription factor NF-kappaB at a concentration of 5 microm and 10 microM in Jurkat T and Raw 264.7 cells, respectively. Elastase release from human neutrophils was reduced to 50% at a concentrations of 23 microM after stimulation with PAF and of 27 microM after stimulation with fMLP without showing cytotoxic effects. Additionally, elastase was also directly inhibited.
The synergistic insecticidal action of characteristic defensive substances produced by the plant family Asteraceae was investigated under controlled laboratory conditions. Sesquiterpene lactones isolated from Asteraceae that may form, through a Michael addition process, conjugates with glutathione were administered in a meridic diet to a herbivorous insect, Manduca sexta. By administering sesquiterpenes, variable in vivo reduced glutathione levels were observed in the insect larvae. When the Asteraceae-derived photooxidant alpha-terthienyl was co-administered, lipid peroxidation and larval mortality were significantly enhanced in the treated groups of insects with lowered in vivo glutathione levels.
Some informations about the sesquiterpene lactones isolated from Brazilian species of Vernonia are described, as well the results of tests developed with such compounds with respect to their anti-feedant, molluscicide, antimicrobial and analgesic properties.
The efficacy of pour-on formulations of three macrocyclic lactone endectocides (moxidectin, ivermectin, and eprinomectin) was evaluated on cattle against Boophilus microplus (Canestrini) using two different treatment regimes. A single application treatment regime with each endectocide showed that fewer ticks per calf were recovered from all treated calves than from untreated cattle, but the level of control among the three treatments was similar (range; 78.7-87.7%) against all stages of ticks on the calves at the time of treatment. The engorged female and egg mass weights of all treated ticks were less than that of untreated ticks. Among the treated groups, the ivermectin and eprinomectin-treated females weighed less and produced lower weight egg masses than those from moxidectin-treated cattle. In a double application treatment regime with a 4-d interval between treatments, there were fewer ticks per calf recovered from the treated cattle than from untreated cattle. In addition, all treated females weighed less and produced lower weight egg masses than those from untreated cattle. Control with moxidectin (90.3%) was lower than with either ivermectin (98.9%) or eprinomectin (99.7%). The mean female and egg mass weight of the ivermectin and eprinomectin-treated groups was also less than that of the moxidectin treatment. A single application treatment against either 18- or 20-d-old adult ticks indicated that both moxidectin and ivermectin were less effective against 20-d-old ticks that were nearer to completing their parasitic development on the animal. In contrast, eprinomectin was the only endectocide tested that was equally effective against both 18- and 20-d-old ticks.
Here, we report an inhibitory effect of a sesquiterpene lactone dehydroleucodine (DhL) on the growth of Trypanosoma cruzi in culture. At concentrations of the drug between 5 and 10 microg/ml in the medium,the parasites remained alive for at least 4 days. Higher concentrations of DhL were lethal for the parasites within a few hours. The effect of DhL is irreversible. Morphological changes induced by DhL were also observed in the parasites. The effect of DhL was blocked by the presence of reducing substrates such as glutathione or dithiothreitol, but these agents were not able to reverse the effect of DhL if added 2 days after the start of drug exposure.
Homogentisic acid gamma-lactone (HAL) chemiluminescence (CL) was applied to the determination of horseradish peroxidase (HRP) encapsulated in liposomes. HRP was detected after the lysis of HRP-trapped liposomes with Triton X-100. CL response rate, detection limit and linear range of calibration curve for HRP in HAL CL were compared with those in piodophenol (p-IP)-enhanced luminol CL. Maximal light emission in HAL CL appeared more rapidly compared to that in p-IP enhanced luminol CL, thus resulting in remarkable reduction of CL measurement time. The detection limit for HRP in HAL CL was the same as that in p-IP-enhanced luminol CL. The linear range of calibration curve for HRP in HAL CL was improved by a factor of 50 compared with that in p-IP-enhanced luminol CL. From these results, it was found that HAL CL were superior to p-IP-enhanced luminol CL for the determination of HRP encapsulated in liposomes.
Belactins A and B, new inhibitors of serine carboxypeptidase were discovered in the fermentation broth of Saccharopolyspora sp. MK19-42F6. The structures of belactins A and B were determined to be 4-[3-[(2-amino-5-chlorobenzoyl)amino]-1,1-dimethyl-2-oxobutyl]-3- methyl-2-oxetanone and 4-[3-[[2-(beta-glucopyranosylamino)-5-chlorobenzoyl]amino]-1,1- dimethyl-2-oxobutyl]-3-methyl-2-oxetanone respectively by various spectral analyses. Belactins A and B do not inhibit esterase or lipase at 100 micrograms/ml but have more specific inhibitory activities towards carboxypeptidase Y (CP-Y) compared with other beta-lactone-containing inhibitors, such as ebelactones A, B and esterastin.
The isolation, biological properties and structure elucidation of a sixteen-membered macrocyclic lactone antibiotic, designated A26771B (1), obtained from Penicillium turbatum are discussed.
Skeletal structure of copiamycin (1) (C54H95N3O17), a potent antifungal antibiotic, was determined from the physicochemical properties of this compound and of its degradation products. This compound consists of 32-membered polyhydroxy lactone ring, an alpha, beta-unsaturated ester group, as well as a side chain with a disubstituted guanidine moiety as its terminal. One of the hydroxyl groups (presumably at C-19) forms a hemiketal ring with the keto group at C-15, and another (at either C-21 or C-23) forms a hemiester with a malonic acid moiety.
Over one million bacteria were isolated from a large variety of soil, plant and water samples collected from different environments and examined in an extremely sensitive and highly specific screen for beta-lactam production. A group of seven related monocyclic beta-lactams (monobactams) were isolated from strains representing four genera-Agrobacterium, Chromobacterium, Gluconobacter and Pseudomonas. Monobactam-producing strains of Agrobacterium and Pseudomonas were isolated only rarely. Producing strains of Chromobacterium were isolated from a relatively limited number of habitats while the Gluconobacter strains appeared to be widespread in nature. In addition, three closely related beta-lactone-containing molecules were isolated from strains representing three genera-Arthrobacter, Bacillus and Pseudomonas. The Bacillus and Pseudomonas strains were isolated infrequently but from a variety of samples. The producing strain of Arthrobacter was isolated only once.
Bacillus subtilis C-756 produced three kinds of inhibitors of cyclic adenosine 3',5'-monophosphate (cAMP) phosphodiesterase. Each was an acylpeptide consisting of a beta-hydroxy fatty acid residue and heptapeptide. By the application of mass spectrometry, the amino acid sequence of peptide was determined to be beta-hydroxy fatty acid-Glu-Leu-Leu-Val-Asp-Leu-Leu in all three cases. Each had a lactone linkage between the carboxyl group of C-terminal leucine and the beta-hydroxyl group of the fatty acid moiety. The total structures of these inhibitors were thus established.
During our screening program for natural product drugs effective against multidrug-resistant mammalian cells, we have discovered a new delta lactone FD-211 from the fermantation broth of Myceliophthora lutea TF-0409. FD-211 had a broad spectrum activity against cultured tumor cell lines, including adriamycin-resistant HL-60 cells.
During the course of our screening for natural products from fungi, extracts of several cultures were found to make a family of related resorcylic acid lactone compounds, which are potent inhibitors of MEK kinase. Comparative and empirical studies of fermentation conditions improved the titers of the compounds of interest. Striking changes in the ratios and amounts of the major and minor compounds in some cases were achieved by manipulations of media composition.
A novel bacterium designated as Aeromonas sp. W-10 produces the antibiotic W-10 complex which comprises of two major and several minor components. The two major components from this complex, Sch 20562 (1) and Sch 20561 (1a), are of biological interest in view of their potent antifungal activity. The chemical degradation studies utilized for the assignment of structure 1 for Sch 20562 are described here. Some of the noteworthy diversity of structural features in this glucosidic cyclic dehydrononapeptide lactone 1 are: an N-terminal (D)-beta-hydroxymyristyl unit, three D-amino acid units, two (E)-alpha-aminocrotonyl units, and an O-alpha-D-glucosyl-N-methyl-L-allo-threonine unit. The structure determination of 1 utilized the selective cleavage of the dehydropeptide units by ozonolysis to form fragments that were sequenced by mass spectrometry. The stereochemistry of the amino acid units were assigned by isolation of the free amino acids from the hydrolysates of the fragments. The stereochemistry of the alpha-aminocrotonyl units and the glucosidic linkage were assigned by nmr spectroscopy and molecular rotation data.
A novel 16-membered lactone antibiotic named tubelactomicin A was isolated from the culture broth of an actinomycete strain. The producing organism, designated MK703-102F1, was identified as a member of Nocardia. Tubelactomicin A was isolated from the culture broth by Diaion HP20 absorption, ethyl acetate extraction, silica gel and Sephadex LH-20 column chromatographies and centrifugal liquid-liquid partition chromatography (CPC). Tubelactomicin A showed strong activity against acid-fast bacteria including the drug-resistant strains.
A novel 16-membered lactone antibiotic named tubelactomicin A was isolated from the culture broth of Nocaradia sp. MK703-102F1. The structure of tubelactomicin A was assigned by spectroscopic analysis and the absolute configuration was determined by X-ray crystallographic analysis.
AIM: To study the effect of Coriaria lactone (CL) on cytosolic free calcium ([Ca2+]i) of cultured neurons from cerebral cortex. METHODS: Primary neuron culture (14d) and AR-CM-MIC cation measurement system were used, the [Ca2+]i were measured. CL effect was observed by loading egtazic acid. RESULTS: The [Ca2+]i of cultured neurons (99.4-103.4) nmol.L-1 was elevated concentration-dependently by CL (25-500) mumol.L-1 (P < 0.01). This effect disappeared after loading egtazic acid 5 mmol.L-1, but reappeared after adding CaCl2 to 1 mmol.L-1. CONCLUSION: The [Ca2+]i of cultured neurons was elevated by CL, depending on extracellular Ca2+.